Disease & Drug Info

Drug Dictionary

G207

A neuroattenuated, replication-competent, recombinant herpes simplex virus-1 (HSV-1) with potential oncolytic activity. Upon intracerebral administration, oncolytic HSV-1 G207 preferentially replicates within glioma cells, which may elicit tumor-specific systemic immune and cytotoxic Tlymphocyte (CTL) responses in addition to direct cytopathic effects. Derived from wild-type HSV-1 strain F, this agent has been neuroattenuated by deletionsin both copies of the gamma34.5 gene, the major determinant of HSVneurovirulence. In addition, the HSV-1 gene UL39, encoding the viral ribonucleotide reductase large subunit infected cell protein 6 (ICP6), has been inactivated through the insertion of the Escherichia coli lacZ gene. By inactivating UL39, viral ribonucleotide reductase activity is disrupted, resulting in the inhibition of nucleotide metabolismand viral DNA synthesis in nondividing cells but not individing cells. Check for active clinical trials using this agent. (NCI Thesaurus)

G250 peptide vaccine

A cancer vaccine containing of a synthetic form of the renal cell carcinoma (RCC)-associated antigen G250 with potential antineoplastic activity. Vaccination with G250 peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells positive for the G250 antigen, resulting in decreased tumor growth. Found in the majority of renal cell carcinomas, G250 is a cell surface tumor-associated antigen (TAA) that contains an HLA-A2.1-restricted epitope that is recognized by CTLs. Check for active clinical trials using this agent. (NCI Thesaurus)

Ga-68-labeled F(ab') 2- trastuzumab

A radioimmunoconjugate consisting of a trastuzumab fragment labeled with the positron-emitting radioisotope gallium Ga 68 with radioisotopic and antibody activities. Upon administration, Ga-68-labeled F(ab')2-trastuzumab may bind to HER2-positive tumor cells, allowing radioimmunolocalization with positron emission tomography (PET). Trastuzumab is a recombinant humanized monoclonal antibody that selectively binds to the extracellular domain of human epidermal growth factor receptor 2 (HER2), overexpressed by many adenocarcinomas, particularly breast adenocarcinomas. Check for active clinical trials using this agent. (NCI Thesaurus)

gabapentin

A synthetic analogue of the neurotransmitter gamma-aminobutyric acid with anticonvulsant activity. Although its exact mechanism of action is unknown, gabapentin appears to inhibit excitatory neuron activity. This agent also exhibits analgesic properties. Check for active clinical trials using this agent. (NCI Thesaurus)

Gadavist

(Other name for: gadobutrol)

gadobenate dimeglumine

A gadolinium-based paramagnetic contrast agent. When placed in a magnetic field, gadobenate dimeglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI. Check for active clinical trials using this agent. (NCI Thesaurus)

gadobutrol

A gadolinium-based, hydrophilic, macrocyclic, electricallyneutral contrast agent used in contrast-enhanced MRI (CE-MRI). Gadobutrol is a non-ionic, paramagnetic complex consisting of gadolinium (Gd3+) chelated with the macrocyclic compound dihydroxy-hydroxymethylpropyl-tetraazacyclododecane-triacetic acid (butrol). Following intravenous administration, gadobutrol may increase MRI sensitivity for the detection of tumors and inflammatory and demyelinating diseases of the central nervous system (CNS) which are associated with areas with blood-brainbarrier defects due to altered perfusion or an enlarged extracellular space. This agent is eliminated in an unchanged form via the kidneys; extra-renal elimination is negligible. Check for active clinical trials using this agent. (NCI Thesaurus)

gadodiamide

A paramagnetic gadolinium-based contrast agent (GBCA), with imaging activity upon magnetic resonance imaging (MRI). When placed in a magnetic field, gadodiamide generates a large local magnetic field, which can enhance the relaxation rate of nearby protons. This change in proton relaxation dynamics, iincreases the MRI signal intensity of tissues in which gadodiamide has accumulated; therefore, visualization of those tissues is enhanced. Check for active clinical trials using this agent. (NCI Thesaurus)

gadofosveset trisodium

The trisodium salt form of gadofosveset, an injectable, intravascular, amphiphilic gadolinium-based contrast agent (GBCA) used with magnetic resonance angiography (MRA) imaging. Gadofosveset is a stable gadolinium diethylenet triaminepentaacetic acid (Gd-DTPA) chelate derivative with a diphenylcyclohe xylphosphate group. Upon injection, gadofosveset binds reversibly to endogenous serum albumin which increases its intravascular retention time compared to non-protein binding contrast agents. The serum albumin binding also increases T1-relaxivity of gadofosveset. This produces an increase in signal intensity of blood, thereby enhancing the visualization of blood vessels upon MRA and may aid in the diagnosis of certain blood vessels and heart disorders. Check for active clinical trials using this agent. (NCI Thesaurus)

gadolinium-chelate

A coordination complex consisting of a gadolinium ion bound to a hexadentate organic chelating agent such as diethylenetriaminepentaacetic acid. Chelates of gadolinium are frequently utilized as magnetic resonance imaging (MRI) contrast agents and can be used to track nanoparticle-mediated drug delivery. Check for active clinical trials using this agent. (NCI Thesaurus)

gadopentetate dimeglumine

A gadolinium complex of diethylenetriamine pentaacetic acid with ionic paramagnetic properties. Gadopentetate dimeglumine may provide contrast enhancement during magnetic resonance imaging (MRI) of intracranial lesions with abnormal vascularity or of abnormalities in the blood-brain barrier (BBB). Check for active clinical trials using this agent. (NCI Thesaurus)

gadoterate meglumine

A gadolinium chelate paramagnetic contrast agent. When placed in a magnetic field, gadoterate meglumine produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because gadobenate dimeglumine is excreted in the bile, it may be used to visualize the biliary system using MRI. Check for active clinical trials using this agent. (NCI Thesaurus)

Gadovist

(Other name for: gadobutrol)

gadoxetate disodium

A paramagnetic contrast agent consisting of the disodium salt of the gadolinium ion chelated with the lipophilic moiety ethoxybenzyl (EOB) bound to diethylenetriamine pentaacetic acid (DTPA). When placed in a magnetic field, gadolinium produces a large magnetic moment and so a large local magnetic field, which can enhance the relaxation rate of nearby protons; as a result, the signal intensity of tissue images observed with magnetic resonance imaging (MRI) may be enhanced. Because this agent is preferentially taken up by normal functioning hepatocytes, normal hepatic tissue is enhanced with MRI while tumor tissue is unenhanced. In addition, because this agent is excreted in the bile, it may be used to visualize the biliary system using MRI. Check for active clinical trials using this agent. (NCI Thesaurus)

Gag:267-274 peptide vaccine

A peptide vaccine containing the amino acids 267 through 274 of the human immunodeficiency virus type 1 (HIV-1) gag core protein (gag:267-274), with potential immunostimulating activity. Upon vaccination, the immune system may exert a potent cytotoxic T-lymphocyte (CTL) response against the xenoantigen gag:267-274 and produces pro-inflammatory cytokines. The concomitant administration of a cancer peptide vaccine may benefit from an already activated immune system and may augment an immune response against the administered tumor associated antigen(s). Gag:267-274 peptide is highly immunogenic and may potentially be used as a cancer immunoadjuvant. Check for active clinical trials using this agent. (NCI Thesaurus)

galactomannan derivative

A carbohydrate polymer composed of mannose and galactose, with chemotherapeutic enhancing activity. Galactomannan derivative binds to galectins on cell surfaces and may promote the transport of certain chemotherapeutics, such as 5-fluorouracil (5-FU), into tumor cells. This may increase the antineoplastic effect of 5-FU when administered concomitantly. Galectins are carbohydrate-binding proteins, upregulated on the surface of certain types of tumor cells, and may mediate cell association, survival and metastasis. Check for active clinical trials using this agent. (NCI Thesaurus)

galactose

A hexose which is almost identical to glucose except that orientation of -H and -OH on carbon 4 are exchanged, making it an epimer at C-4 of glucose (in Fisher projection). Check for active clinical trials using this agent. (NCI Thesaurus)

galantamine hydrobromide

The hydrobromide salt form of galantamine, a tertiary alkaloid obtained synthetically or naturally from the bulbs and flowers of Narcissus and several other genera of the Amaryllidaceae family with anticholinesterase and neurocognitive-enhancing activities. Galantamine competitively and reversibly inhibits acetylcholinesterase, thereby increasing the concentration and enhancing the action of acetylcholine (Ach). In addition, galantamine is a ligand for nicotinic acetylcholine receptors, which may increase the presynaptic release of Ach and activate postsynaptic receptors. This agent may improve neurocognitive function in mild and moderate Alzheimer' s disease and may reduce abstinence-induced cognitive symptoms that promote smoking relapse. Check for active clinical trials using this agent.

galectin inhibitor GR-MD-02

A carbohydrate-based galectin inhibitor, with potential antineoplastic activity. Galectin inhibitor GR-MD-02 binds to the carbohydrate-binding domain of galectins, especially galectin-3, and may result in an induction of apoptosis mediated through activation of both mitochondria and caspases. This may reduce tumor growth in galectin-overexpressing tumor cells. Galectins, often overexpressed on tumor cells, play a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)

galectin-1 inhibitor OTX008

A calixarene-based compound and galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. Upon subcutaneous administration, galectin-1 inhibitor OTX008 binds Gal-1 which leads to Gal-1 oxidation and proteosomal degradation through a not yet fully elucidated mechanism, and eventually downregulates Gal-1. This decreases tumor cell growth and inhibits angiogenesis. Gal-1, a multifunctional carbohydrate-binding protein, is often overexpressed on tumor cells and plays a key role in cancer cell proliferation, apoptosis, tumor angiogenesis and evasion of immune responses. Check for active clinical trials using this agent. (NCI Thesaurus)

galeterone

An orally bioavailable small-molecule androgen receptor modulator and CYP17 lyase inhibitor with potential antiandrogen activity. Galeterone exhibits three distinct mechanisms of action: 1) as an androgen receptor antagonist, 2) as a CYP17 lyase inhibitor and 3) by decreasing overall androgen receptor levels in prostate cancer tumors, all of which may result in a decrease in androgen-dependent growth signaling. Localized to the endoplasmic reticulum (ER), the cytochrome P450 enzyme CYP17 (P450C17 or CYP17A1) exhibits both 17alpha-hydroxylase and 17,20-lyase activities, and plays a key role in the steroidogenic pathway that produces progestins, mineralocorticoids, glucocorticoids, androgens, and estrogens. Check for active clinical trials using this agent. (NCI Thesaurus)

galiximab

A humanized IgG1 monoclonal antibody directed against CD80, the natural ligand for the T-cell antigen CD28 which mediates T-cell and B-cell adhesion. Galiximab binds to CD80 expressed on the cell surfaces of follicular lymphomas, resulting in antibody-dependent cell-mediated cytotoxicity (ADCC). CD80 is expressed on activated B-cells and gamma-interferon-stimulated monocytes and is often expressed at low levels on the surfaces of follicular lymphoma cells and other lymphoid malignancies. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium citrate Ga 67

The citrate salt of the radioisotope gallium Ga 67. Although the mechanism is unknown, gallium Ga 67 concentrates in lysosomes and is bound to a soluble intracellular protein in certain viable primary and metastatic tumors and focal sites of inflammation, allowing scintigraphic localization. Ga-67 scintigraphy (GS) cannot differentiate between tumor and acute inflammation. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68 citrate

A radiopharmaceutical citrate salt form of the positron-emitting radioisotope gallium Ga 68, with potential imaging activity upon positron emission tomography (PET). Upon administration of Gallium Ga 68 citrate, the gallium Ga 3+ ion dissociates from the weak citrate chelator. As Ga3+ is very similar to iron (Fe3+) in chemical properties, this ion acts as an iron analogue. Ga3+ binds to the iron-binding protein transferrin, distributes in blood, and enters and accumulates in the extracellular fluid space of inflamed or tumor-bearing tissue. In turn, the Ga3+-transferrin complex binds to transferrin receptors and is taken up by tumor cells. Tumor cells can then be imaged upon PET. Compared to healthy cells, tumor cells have increased iron metabolism and transferrin receptor expression. Increased Ga3+ uptake is seen in inflamed and infected tissues as well. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68 OPS202

A radioconjugate consisting of the somatostatin antagonistic peptide OPS202 that is labeled with the positron-emitting radionuclide gallium Ga 68, which may be used as a somatostatin receptor (SSTR) imaging agent in conjunction with positron emission tomography (PET) to image neuroendocrine tumors (NETs). Gallium Ga 68 OPS202 binds to SSTR subtype 2 present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive cells upon imaging. SSTR subtypes have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTR subtypes. Check for active clinical trials using this agent.

gallium Ga 68-DOTA-exendin-4

A radiopharmaceutical composed of the glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4 linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the positron-emitting radionuclide gallium Ga 68, with potential use in diagnostic imaging upon positron emission tomography (PET). Upon administration of gallium Ga 68-DOTA-exendin-4, the exendin-4 moiety binds to GLP-1R and is subsequently internalized. The radionuclide moiety can be detected using PET and GLP-1R-expressing tumors can be localized. GLP-1R, located on beta cells, is overexpressed on insulinomas, which are insulin-secreting neuroendocrine tumors. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-DOTANOC

A gallium Ga 68-radiolabeled analogue of somatostatin that may be used in conjunction with positron emission tomography (PET) to image neuroendocrine tumors and metastases. Gallium Ga 68-DOTANOC is a conjugate of the somatostatin analogue 1-Nal3-octreotide (NOC) and gallium Ga 68-labeled 1,4,7,10-tetraazacyclododecane-N,N',N'',N'''-tetraacetic acid (DOTA). The somatostatin analogue NOC has a high affinity for somatostatin receptor subtypes 2, 3, and 5; these receptor subtypes have been shown to be present in large numbers on neuroendocrine tumors and their metastases, while most other normal tissues express low levels of these somatostatin receptor subtypes. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-DOTATATE

A radioconjugate consisting of the somatostatin analogue tyrosine-3-octreotate (Tyr3-octreotate or TATE) labeled with the positron emission tomography (PET) tracer gallium Ga 68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA), which may be used as a somatostatin receptor (SSTR) imaging agent in conjunction with PET to image neuroendocrine tumors (NETs). Gallium Ga 68-DOTATATE binds to SSTRs, with a much higher affinity for type 2 SSTR, present on the cell membranes of many types of NETs. This allows for visualization of SSTR-positive cells upon imaging. SSTR subtypes have been shown to be present in large numbers on NETs and their metastases, while most other normal tissues express low levels of SSTR subtypes. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-edotreotide

A radioconjugate consisting of the octreotide derivative edotreotide labeled with gallium 68 (Ga-68) with potential application in somatostatin receptor (SSTR) imaging in conjunction with positron emission tomography (PET). Similar to octreotide, gallium Ga 68-edotreotide binds to SSTRs, especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells and their metastases, thereby allowing for imaging of SSTR-expressing cells upon PET. Gallium Ga 68-edotreotide is produced by substituting tyrosine for phenylalanine at the 3 position of the somatostatin analogue octreotide (Tyr3-octreotide or TOC) and chelating the substituted octreotide to Ga-68 via the macrocyclic chelating agent dodecanetetraacetic acid (DOTA). Check for active clinical trials using this agent.

gallium Ga 68-labeled affibody molecule ABY-025

A radioconjugate composed of an optimized affibody conjugated, via its C-terminal cysteine, to maleimide-DOTA, and linked to the radioisotope gallium Ga 68, with potential use as a tracer for human epidermal growth factor receptor type 2 (HER2; ErbB2)-expressing tumors using positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68-labeled affibody ABY-025, the affibody targets HER2-expressing tumor cells. This facilitates both detection of HER2-expressing tumor cells and assessment of responses to HER2-targeting chemotherapeutic agents during PET imaging. The affibody is an optimized antibody mimetic based on a 6.5-kDa 3-helical bundle Z domain derived from the staphylococcal protein A (Z her2:342); the nonbinding surface of the Z domain is reengineered (Z her2:2891) to increase binding affinity for HER2 and to improve tumor imaging. HER2 is overexpressed in many cancer cell types. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-labeled BNOTA-PRGD2

A radiopharmaceutical agent comprised of a pegylated arginine-glycine-aspartic acid dimer (PRGD2) labeled with gallium Ga 68, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET) or single photon emission computed tomography (SPECT). This radiopharmaceutical is prepared by conjugating PRGD2 with chelator S-2-(4-isothiocyanatobenzyl)-1,4,7-triazacyclononane-1,4,7-triacetic acid (BNOTA) which is capable of forming a six-coordinate complex with Ga 68. After intravenous administration, gallium Ga 68-labeled BNOTA-PRGD2 binds to alphaVbeta3 integrin on the cell membrane via the cyclic tri-amino acids RGD motif. Upon PET imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. Compared to other radiolabeled RGD-containing peptides, this agent shows increased affinity to alphaVbeta3 integrin, enhanced tumor uptake as well as improved pharmacokinetics. alphaVbeta3 integrin is overexpressed on certain tumor cells and tumor endothelial cells while minimally or not expressed on healthy, normal cells and plays a key role in angiogenesis, tumor proliferation and survival. Check for active clinical trials using this agent.

gallium Ga 68-labeled DOTA Di-HSG peptide IMP-288

A radiolabeled divalent histamine-succinyl-glycine (HSG) hapten-peptide linked with the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide gallium (Ga) 68 with potential use in diagnostic imaging. After pretargeting with a bispecific monoclonal antibody (BiMoAB) directed against both a tumor-associated antigen (TAA) and the HSG hapten-peptide, the HSG portion of administered gallium Ga 68-labeled di-HSG-DOTA peptide IMP-288 binds the anti-HSG portion of the BiMoAB; Ga-68 radioisotopic activity localized to tumor cells bearing the TAA can then be visualized upon positron emission tomography (PET). Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-labeled GRPR antagonist BAY86-7548

A radioconjugate containing a synthetic bombesin receptor antagonist targeting the gastrin-releasing peptide receptor (GRPR), that is linked by the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68 GRPR antagonist BAY86-7548, the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor 2 (BB2), is a G protein-coupled seven-transmembrane receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-labeled MLN6907

A radioconjugate containing a monoclonal antibody directed against guanylyl cyclase C (GCC) labeled with the radioisotope gallium Ga 68, with positron emission tomography (PET) imaging activity. The monoclonal antibody moiety of MLN6907 selectively binds to GCC, a transmembrane receptor normally found on intestinal cells and dopaminergic neurons in the brain, that is also overexpressed on the surface of a variety of cancer cells. Upon internalization of the agent and PET, tumors expressing GCC can be visualized. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-labeled NODAGA-MJ9

A radiopharmaceutical agent comprised of a peptide targeting the gastrin releasing peptide receptor (GRPR) chelated with 1,4,7-triazacyclononane,1-glutaric acid-4,7 acetic acid (NODAGA) and radiolabeled with gallium Ga 68, with potential tumor imaging activity upon positron emission tomography (PET). After administration of gallium Ga 68-labeled-NODAGA-MJ9, the MJ9 moiety binds to GRPR located on tumor cells. Upon PET imaging, GRPR-expressing tumor cells can be visualized and expression levels can be quantified. GRPR is overexpressed on certain tumor cells and plays a key role in tumor proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-labeled PSMA ligand Glu-urea-Lys(Ahx)

A radioconjugate composed of a human prostate specific membrane antigen (PSMA)-targeting ligand, Glu-urea-Lys(Ahx) (Glu-NH-CO-NH-Lys(Ahx)), conjugated, via the acyclic radiometal chelator N,N'-bis [2-hydroxy-5-(carboxyethyl)benzyl] ethylenediamine-N,N'-diacetic acid (HBED-CC), to the radioisotope gallium Ga 68, with potential use as a tracer for PSMA-expressing tumors during positron emission tomography (PET). Upon intravenous administration of the gallium Ga 68-labeled PSMA ligand, the Glu-urea-Lys(Ahx) moiety targets and binds to PSMA-expressing tumor cells. Upon internalization, PSMA-expressing tumor cells can be detected during PET imaging. PSMA, a tumor-associated antigen and type II transmembrane protein, is expressed on the membrane of prostatic epithelial cells and overexpressed on prostate tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-NEB

A radiotracer composed of a truncated form of the azo dye Evans blue (EB) conjugated, via a 1,4,7-triazacyclononane-N,N',N"-triacetic acid (NOTA) linker (NEB), to the radioisotope gallium Ga 68, with potential blood pool imaging activity for use in positron emission tomography (PET). Upon administration of gallium Ga 68-NEB, the NEB moiety, which has high affinity for serum albumin, targets and forms a complex with albumin. Upon PET, the lymph nodes (LN) and lymphatic vessels as well as other desired tissues can be visualized. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-NOTA-Aca-BBN(7-14)

A radioconjugate containing the bombesin (BBN) fragment BBN(7-14) comprised of the amino acid sequence of Gln-Trp-Ala-Val-Gly-His-Leu-Met-NH2, which targets the gastrin-releasing peptide receptor (GRPR), bound to aminocaproic acid (Aca), and linked by the macrocyclic chelating agent, 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA), to the radionuclide gallium (Ga) 68, with potential use in diagnostic imaging using positron emission tomography/computed tomography (PET/CT). Upon administration of gallium Ga 68-NOTA-Aca-BBN(7-14), the peptide moiety targets and binds to GRPR. Upon PET/CT, GRPR-expressing tumor cells can then be visualized. GRPR, also called bombesin receptor 2 (BB2), is a seven-transmembrane G protein-coupled receptor belonging to the bombesin receptor family. It is overexpressed in certain types of cancers. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-NOTA-AE105

A radiotracer composed of AE105, an urokinase-type plasminogen activator receptor (uPAR) peptide antagonist, conjugated with the bifunctional, macrocyclic chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and labeled with the radionuclide gallium Ga 68, with potential imaging activity using positron emission tomography (PET). Upon administration, the AE105 moiety of gallium Ga 68-NOTA-AE105 targets and binds, with high affinity, to uPAR expressed on tumor cells. Upon PET imaging, uPAR-expressing tumor cells can be visualized and the degree of tumor aggressiveness can be assessed. uPAR expression is correlated with increased tumor invasiveness and aggressiveness, as well as a poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)

gallium Ga 68-NOTA-NFB

A radioconjugate composed of a derivative of the CXCR4 peptide antagonist T140, in which the N-terminal 4-fluoro-benzoyl group (NFB) is substituted with the chelating agent 1,4,7-triazacyclononane-N,N',N''-triacetic acid (NOTA) and radiolabeled with gallium Ga 68, with potential CXCR4 imaging activity during positron emission topography (PET). Upon administration, gallium Ga 68-NOTA-NFB selectively binds to CXCR4 and CXCR4-expressing tumor cells can then be visualized upon PET imaging. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis, and is upregulated in several tumor cell types. CXCR4 expression is correlated with tumor aggressiveness and high metastatic potential. Unmodified T140 binds non-specifically to red blood cells (RBCs); replacing the fluoro-benzoyl group with NOTA (NOTA-NFB) prevents the RBC binding almost entirely, while only minimally reducing the binding to CXCR4-positive tumor cells. Check for active clinical trials using this agent. (NCI Thesaurus)

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